- Organic compounds
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The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar′, A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.
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Page/Page column 46
(2009/10/01)
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- THIAZOLIUMS AS TRANSKETOLASE INHIBITORS
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The present invention provides N-3'-pyridylmethyl or N-2'-pyrazinylmethyl thiazolium derivatives of formula (I) which are useful as transketolase inhibitors wherein R1, R2, R3, Y, R5-R9, Ra-Rd, n and X- are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.
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Page/Page column 39
(2008/06/13)
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- Research on heterocyclic compounds. XXXVII. Synthesis and antiinflammatory activity of methyl-substituted imidazo[1,2-a]pyrazine derivatives
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A series of methyl-substituted imidazo[1,2-a]pyrazines 8 bearing a carboxylic acid group on the imidazole ring were synthesized. The structures of new compounds were confirmed by 1H- and 13C-NMR spectral data; the correct assignment of carbon resonances was made by means of HETCOR and COLOC experiments. Antiinflammatory, analgesic and ulcerogenic activities in vivo were evaluated and compared with those of antiinflammatory imidazopyrazines (2 and 3) and indomethacin. The inhibitory action on cyclooxygenase activity was evaluated in vitro. Compounds 8 were found to be less potent than indomethacin in these assays. SARs are discussed.
- Rimoli,Avallone,De Caprariis,Luraschi,Abignente,Filippelli,Berrino,Rossi
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p. 195 - 203
(2007/10/03)
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